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1 August 2021
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Cover Image
The hERG1 potassium channel is found on pathological tissue, such as many cancers, as well as non-pathological tissue such as the heart. By generating a bispecific antibody in the form of a single-chain diabody (scDb) to both the hERG1 channel and the β1 subunit of integrin receptors, Duranti and colleagues have created a potent therapeutic with good pharmacokinetics and no observed cardiac or renal toxicity. Read the full article on page 1338. - PDF Icon PDF LinkTable of Contents
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ISSN 1535-7163
EISSN 1538-8514
Highlights
MCT First Disclosures
ASN004, A 5T4-targeting scFv-Fc Antibody–Drug Conjugate with High Drug-to-Antibody Ratio, Induces Complete and Durable Tumor Regressions in Preclinical Models
Roger A. Smith; David J. Zammit; Nitin K. Damle; Helen Usansky; Sanjeeva P. Reddy; Jun-Hsiang Lin; Mahesh Mistry; Niranjan S. Rao; Louis J. Denis; Sandeep Gupta
Harnessing the hERG1/β1 Integrin Complex via a Novel Bispecific Single-chain Antibody: An Effective Strategy against Solid Cancers
Claudia Duranti; Jessica Iorio; Tiziano Lottini; Elena Lastraioli; Silvia Crescioli; Giacomo Bagni; Matteo Lulli; Chiara Capitani; Rayhana Bouazzi; Matteo Stefanini; Laura Carraresi; Luisa Iamele; Hugo De Jonge; Annarosa Arcangeli
Reviews
Small Molecule Therapeutics
Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models
Danlin Sun; Anna S. Nikonova; Peishan Zhang; Alexander Y. Deneka; Mark E. Fitzgerald; Ryan E. Michael; Linda Lee; Anna C. Lilly; Stewart L. Fisher; Andrew J. Phillips; Christopher G. Nasveschuk; David A. Proia; Zhigang Tu; Erica A. Golemis
M3258 Is a Selective Inhibitor of the Immunoproteasome Subunit LMP7 (β5i) Delivering Efficacy in Multiple Myeloma Models
Michael P. Sanderson; Manja Friese-Hamim; Gina Walter-Bausch; Michael Busch; Stefanie Gaus; Djordje Musil; Felix Rohdich; Ugo Zanelli; Sondra L. Downey-Kopyscinski; Constantine S. Mitsiades; Oliver Schadt; Markus Klein; Christina Esdar
CSF1/CSF1R Signaling Inhibitor Pexidartinib (PLX3397) Reprograms Tumor-Associated Macrophages and Stimulates T-cell Infiltration in the Sarcoma Microenvironment
Tomohiro Fujiwara; Mohamed A. Yakoub; Andrew Chandler; Alexander B. Christ; Guangli Yang; Ouathek Ouerfelli; Vinagolu K. Rajasekhar; Aki Yoshida; Hiroya Kondo; Toshiaki Hata; Hiroshi Tazawa; Yildirim Dogan; Malcolm A.S. Moore; Toshiyoshi Fujiwara; Toshifumi Ozaki; Ed Purdue; John H. Healey
Venetoclax-based Rational Combinations are Effective in Models of MYCN-amplified Neuroblastoma
Krista M. Dalton; Kateryna Krytska; Timothy L. Lochmann; Renata Sano; Colleen Casey; Alessia D'Aulerio; Qasim A. Khan; Giovanna Stein Crowther; Colin Coon; Jinyang Cai; Sheeba Jacob; Richard Kurupi; Bin Hu; Mikhail Dozmorov; Patricia Greninger; Andrew J. Souers; Cyril H. Benes; Yael P. Mossé; Anthony C. Faber
Silylation of Deoxynucleotide Analog Yields an Orally Available Drug with Antileukemia Effects
Hiroshi Ureshino; Yuki Kurahashi; Tatsuro Watanabe; Satoshi Yamashita; Kazuharu Kamachi; Yuta Yamamoto; Yuki Fukuda-Kurahashi; Nao Yoshida-Sakai; Naoko Hattori; Yoshihiro Hayashi; Atsushi Kawaguchi; Kaoru Tohyama; Seiji Okada; Hironori Harada; Toshikazu Ushijima; Shinya Kimura
Targeting the T-Cell Lymphoma Epigenome Induces Cell Death, Cancer Testes Antigens, Immune-Modulatory Signaling Pathways
Luigi Scotto; Cristina Kinahan; Eugene Douglass; Changchun Deng; Maryam Safari; Beatrice Casadei; Enrica Marchi; Jennifer K. Lue; Francesca Montanari; Lorenzo Falchi; Changhong Qiao; Nandakumar Renu; Susan E. Bates; Andrea Califano; Owen A. O'Connor
Novel and Highly Potent ATR Inhibitor M4344 Kills Cancer Cells With Replication Stress, and Enhances the Chemotherapeutic Activity of Widely Used DNA Damaging Agents
Ukhyun Jo; Ilya S. Senatorov; Astrid Zimmermann; Liton Kumar Saha; Yasuhisa Murai; Se Hyun Kim; Vinodh N. Rajapakse; Fathi Elloumi; Nobuyuki Takahashi; Christopher W. Schultz; Anish Thomas; Frank T. Zenke; Yves Pommier
Large Molecule Therapeutics
First-in-Human, Phase 1 Dose-Escalation Study of Biparatopic Anti-HER2 Antibody–Drug Conjugate MEDI4276 in Patients with HER2-positive Advanced Breast or Gastric Cancer
Mark D. Pegram; Erika P. Hamilton; Antoinette R. Tan; Anna Maria Storniolo; Kemal Balic; Anton I. Rosenbaum; Meina Liang; Peng He; Shannon Marshall; Anita Scheuber; Mayukh Das; Manish R. Patel
Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers
Gene Expression Signature Correlates with Outcomes in Metastatic Renal Cell Carcinoma Patients Treated with Everolimus Alone or with a Vascular Disrupting Agent
Eddy S. Yang; Amin H. Nassar; Elio Adib; Opeyemi A. Jegede; Sarah Abou Alaiwi; Deborah L. Della Manna; David A. Braun; Mahsa Zarei; Heng Du; Sumanta K. Pal; Gurudatta Naik; Guru P. Sonpavde
Models and Technologies
International Consensus on Minimum Preclinical Testing Requirements for the Development of Innovative Therapies For Children and Adolescents with Cancer
Gilles Vassal; Peter J. Houghton; Stefan M. Pfister; Malcolm A. Smith; Huib N. Caron; Xiao-Nan Li; David J. Shields; Olaf Witt; Jan J. Molenaar; Sara Colombetti; Julia Schüler; Lou F. Stancato
Therapeutic Synergy in Esophageal Cancer and Mesothelioma Is Predicted by Dynamic BH3 Profiling
Deborah R. Surman; Yuan Xu; Min-Jung Lee; Jane Trepel; Kate Brown; Maheshwari Ramineni; Taylor G. Splawn; Laurence P. Diggs; H. Courtney Hodges; Jeremy L. Davis; Hyun-Sung Lee; Bryan M. Burt; Robert Taylor Ripley
Oncolytic Vaccinia Virus Gene Modification and Cytokine Expression Effects on Tumor Infection, Immune Response, and Killing
Tomoyoshi Inoue; Thomas Byrne; Mitsuko Inoue; Madeline E. Tait; Patrick Wall; Annabel Wang; Michael R. Dermyer; Hanane Laklai; Joseph J. Binder; Clare Lees; Robert Hollingsworth; Liliana Maruri-Avidal; David H. Kirn; Donald M. McDonald
Correction
Correction: SMARCB1/INI1 Genetic Inactivation Is Responsible for Tumorigenic Properties of Epithelioid Sarcoma Cell Line VAESBJ
Monica Brenca; Sabrina Rossi; Erica Lorenzetto; Elena Piccinin; Sara Piccinin; Francesca Maria Rossi; Alberto Giuliano; Angelo Paolo Dei Tos; Roberta Maestro; Piergiorgio Modena
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